Preparation method of polygeline-bound paclitaxel nanoparticles

Abstract

The invention provides a preparation method of polygeline-bound paclitaxel nanoparticles. The method comprises the steps of mixing a polygeline solution with a paclitaxel-containing organic solvent, homogenizing, and then freeze-drying, wherein the polygeline solution is used as a water phase, and the paclitaxel-containing organic solvent is taken as an oil phase; the homogenizing process concretely comprises the steps of carrying out emulsification on the mixed solution for 5-120min under 100-600 bar, and then homogenizing for 5-180min under 900-2000 bar. The preparation method, provided by the invention, of the polygeline-bound paclitaxel nanoparticles is high in yield, effectively reduces the cost price of similar products, solves the problems that paclitaxel is poor in water solubilityand low in drug loading capacity, and is suitable for industrialized popularization.

Description

technical field [0001] The invention relates to the technical field of drug nanoparticle carriers, and more specifically, to a method for preparing polygelatin-bound paclitaxel nanoparticles. Background technique [0002] Paclitaxel can be used alone or in combination with other antineoplastic drugs, and can be used clinically to treat breast cancer, ovarian cancer, non-small cell lung cancer, etc. However, paclitaxel is extremely poor in water solubility, and the traditional clinical application of paclitaxel injection requires a mixture of polyoxyethylene castor oil (Cremophor EL) and absolute ethanol as a solubilizer. However, Cremophor EL solvent is easy to introduce a series of allergic reactions, and desensitization treatment is required before administration, which severely limits the use of paclitaxel. Paclitaxel lacks target specificity. As a cytotoxic drug, it will cause severe toxicity and adverse reactions during clinical application, mainly manifested as neutro...

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Problems solved by technology

However, human albumin as an auxiliary material is expensive and has limited sources, which brings a heavy economic burden to patients. The auxiliary material used in the patent US6,749,868 is exactly human albumin. Although the process is simple and easy to industrialize, But excipients are expensive

Although the method described in the patent CN106389383A mentions the preparation of nanoparticles by combining gelatin polypeptide with paclitaxel, on the one hand, the preparation process of the gelatin polypeptide is cumbersome, and the prepared gelatin polypeptide solution still needs to establish quality standards for regulation; on the other hand, The preparation process is easy to cause precipitation and cannot be effectively emulsified and clarified, and the yield is too low. The above determines that the method has the disadvantages of unreasonable formula and difficult industrialization in the preparation of gelatin polypeptide-bound paclitaxel nanoparticles.

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